GW 501516

Research use only, not for human use.

A potent and subtype-selective PPARδ agonist with Ki of 1.1 nM in human PPARδ binding assay.

A potent and subtype-selective PPARδ agonist with Ki of 1.1 nM in human PPARδ binding assay; displays >1,000-fold selectivity over other PPAR subtypes; increases expression of the reverse cholesterol transporter ATP-binding cassette A1 and induces apolipoprotein A1-specific cholesterol efflux in macrophages, fibroblasts, and intestinal cells.Dyslipidemia Phase 2 Discontinued(In Vitro):GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner. (In Vivo):GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ. GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner.

GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats. GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model. GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice.

GW 1516 | GSK-516 | GW-501516

Metabolic Enzyme/Protease

PPAR

PPARδ

Cardiovascular Disease

Dyslipidemia

317318-70-0

453.4977

C21H18F3NO3S2

>98% (HPLC)

10 mM in DMSO

O=C(O)COC1=CC=C(SCC2=C(C)N=C(C3=CC=C(C(F)(F)F)C=C3)S2)C=C1C

Acetic acid, 2-[2-methyl-4-[[[4-methyl-2-[4-(trifluoromethyl)phenyl]-5-thiazolyl]methyl]thio]phenoxy]-

(-20℃)

With Ice Pack

≥ 2 years